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Items: 46

1.

Targeting enhancer switching overcomes non-genetic drug resistance in acute myeloid leukaemia.

Bell CC, Fennell KA, Chan YC, Rambow F, Yeung MM, Vassiliadis D, Lara L, Yeh P, Martelotto LG, Rogiers A, Kremer BE, Barbash O, Mohammad HP, Johanson TM, Burr ML, Dhar A, Karpinich N, Tian L, Tyler DS, MacPherson L, Shi J, Pinnawala N, Yew Fong C, Papenfuss AT, Grimmond SM, Dawson SJ, Allan RS, Kruger RG, Vakoc CR, Goode DL, Naik SH, Gilan O, Lam EYN, Marine JC, Prinjha RK, Dawson MA.

Nat Commun. 2019 Jun 20;10(1):2723. doi: 10.1038/s41467-019-10652-9.

PMID:
31222014
2.

Rational Targeting of Cooperating Layers of the Epigenome Yields Enhanced Therapeutic Efficacy against AML.

Duy C, Teater M, Garrett-Bakelman FE, Lee TC, Meydan C, Glass JL, Li M, Hellmuth JC, Mohammad HP, Smitheman KN, Shih AH, Abdel-Wahab O, Tallman MS, Guzman ML, Muench D, Grimes HL, Roboz GJ, Kruger RG, Creasy CL, Paietta EM, Levine RL, Carroll M, Melnick AM.

Cancer Discov. 2019 May 10. doi: 10.1158/2159-8290.CD-19-0106. [Epub ahead of print]

PMID:
31076479
3.

CARM1 Is Essential for Myeloid Leukemogenesis but Dispensable for Normal Hematopoiesis.

Greenblatt SM, Man N, Hamard PJ, Asai T, Karl D, Martinez C, Bilbao D, Stathias V, Jermakowicz AM, Duffort S, Tadi M, Blumenthal E, Newman S, Vu L, Xu Y, Liu F, Schurer SC, McCabe MT, Kruger RG, Xu M, Yang FC, Tenen DG, Watts J, Vega F, Nimer SD.

Cancer Cell. 2019 Jan 14;35(1):156. doi: 10.1016/j.ccell.2018.12.008. No abstract available.

PMID:
30645972
4.

Histone demethylase LSD1 is required for germinal center formation and BCL6-driven lymphomagenesis.

Hatzi K, Geng H, Doane AS, Meydan C, LaRiviere R, Cardenas M, Duy C, Shen H, Vidal MNC, Baslan T, Mohammad HP, Kruger RG, Shaknovich R, Haberman AM, Inghirami G, Lowe SW, Melnick AM.

Nat Immunol. 2019 Jan;20(1):86-96. doi: 10.1038/s41590-018-0273-1. Epub 2018 Dec 10.

5.

Lysine specific demethylase 1 inactivation enhances differentiation and promotes cytotoxic response when combined with all-trans retinoic acid in acute myeloid leukemia across subtypes.

Smitheman KN, Severson TM, Rajapurkar SR, McCabe MT, Karpinich N, Foley J, Pappalardi MB, Hughes A, Halsey W, Thomas E, Traini C, Federowicz KE, Laraio J, Mobegi F, Ferron-Brady G, Prinjha RK, Carpenter CL, Kruger RG, Wessels L, Mohammad HP.

Haematologica. 2019 Jun;104(6):1156-1167. doi: 10.3324/haematol.2018.199190. Epub 2018 Dec 4.

6.

CARM1 Is Essential for Myeloid Leukemogenesis but Dispensable for Normal Hematopoiesis.

Greenblatt SM, Man N, Hamard PJ, Asai T, Karl D, Martinez C, Bilbao D, Stathias V, McGrew-Jermacowicz A, Duffort S, Tadi M, Blumenthal E, Newman S, Vu L, Xu Y, Liu F, Schurer SC, McCabe MT, Kruger RG, Xu M, Yang FC, Tenen D, Watts J, Vega F, Nimer SD.

Cancer Cell. 2018 Nov 12;34(5):868. doi: 10.1016/j.ccell.2018.10.009. No abstract available.

PMID:
30423301
7.

Activation of the p53-MDM4 regulatory axis defines the anti-tumour response to PRMT5 inhibition through its role in regulating cellular splicing.

Gerhart SV, Kellner WA, Thompson C, Pappalardi MB, Zhang XP, Montes de Oca R, Penebre E, Duncan K, Boriack-Sjodin A, Le B, Majer C, McCabe MT, Carpenter C, Johnson N, Kruger RG, Barbash O.

Sci Rep. 2018 Jun 26;8(1):9711. doi: 10.1038/s41598-018-28002-y.

8.

CARM1 Is Essential for Myeloid Leukemogenesis but Dispensable for Normal Hematopoiesis.

Greenblatt SM, Man N, Hamard PJ, Asai T, Karl D, Martinez C, Bilbao D, Stathias V, Jermakowicz AM, Duffort S, Tadi M, Blumenthal E, Newman S, Vu L, Xu Y, Liu F, Schurer SC, McCabe MT, Kruger RG, Xu M, Yang FC, Tenen DG, Watts J, Vega F, Nimer SD.

Cancer Cell. 2018 Jun 11;33(6):1111-1127.e5. doi: 10.1016/j.ccell.2018.05.007. Erratum in: Cancer Cell. 2018 Nov 12;34(5):868. Cancer Cell. 2019 Jan 14;35(1):156.

9.

MEK inhibitors overcome resistance to BET inhibition across a number of solid and hematologic cancers.

Wyce A, Matteo JJ, Foley SW, Felitsky DJ, Rajapurkar SR, Zhang XP, Musso MC, Korenchuk S, Karpinich NO, Keenan KM, Stern M, Mathew LK, McHugh CF, McCabe MT, Tummino PJ, Kruger RG, Carpenter C, Barbash O.

Oncogenesis. 2018 Apr 20;7(4):35. doi: 10.1038/s41389-018-0043-9.

10.

LSD1 inhibition exerts its antileukemic effect by recommissioning PU.1- and C/EBPα-dependent enhancers in AML.

Cusan M, Cai SF, Mohammad HP, Krivtsov A, Chramiec A, Loizou E, Witkin MD, Smitheman KN, Tenen DG, Ye M, Will B, Steidl U, Kruger RG, Levine RL, Rienhoff HY Jr, Koche RP, Armstrong SA.

Blood. 2018 Apr 12;131(15):1730-1742. doi: 10.1182/blood-2017-09-807024. Epub 2018 Feb 16.

11.

Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma.

Drew AE, Moradei O, Jacques SL, Rioux N, Boriack-Sjodin AP, Allain C, Scott MP, Jin L, Raimondi A, Handler JL, Ott HM, Kruger RG, McCabe MT, Sneeringer C, Riera T, Shapiro G, Waters NJ, Mitchell LH, Duncan KW, Moyer MP, Copeland RA, Smith J, Chesworth R, Ribich SA.

Sci Rep. 2017 Dec 21;7(1):17993. doi: 10.1038/s41598-017-18446-z.

12.

Targeting Histone Methylation in Cancer.

McCabe MT, Mohammad HP, Barbash O, Kruger RG.

Cancer J. 2017 Sep/Oct;23(5):292-301. doi: 10.1097/PPO.0000000000000283. Review.

PMID:
28926430
13.

Antitumor activity of LSD1 inhibitors in lung cancer.

Mohammad HP, Kruger RG.

Mol Cell Oncol. 2016 Jan 6;3(2):e1117700. doi: 10.1080/23723556.2015.1117700. eCollection 2016 Mar.

14.

Structure-Based Design of a Novel SMYD3 Inhibitor that Bridges the SAM-and MEKK2-Binding Pockets.

Van Aller GS, Graves AP, Elkins PA, Bonnette WG, McDevitt PJ, Zappacosta F, Annan RS, Dean TW, Su DS, Carpenter CL, Mohammad HP, Kruger RG.

Structure. 2016 May 3;24(5):774-781. doi: 10.1016/j.str.2016.03.010. Epub 2016 Apr 7.

15.

Corrigendum: The promise and peril of chemical probes.

Arrowsmith CH, Audia JE, Austin C, Baell J, Bennett J, Blagg J, Bountra C, Brennan PE, Brown PJ, Bunnage ME, Buser-Doepner C, Campbell RM, Carter AJ, Cohen P, Copeland RA, Cravatt B, Dahlin JL, Dhanak D, Edwards AM, Frederiksen M, Frye SV, Gray N, Grimshaw CE, Hepworth D, Howe T, Huber KV, Jin J, Knapp S, Kotz JD, Kruger RG, Lowe D, Mader MM, Marsden B, Mueller-Fahrnow A, Müller S, O'Hagan RC, Overington JP, Owen DR, Rosenberg SH, Ross R, Roth B, Schapira M, Schreiber SL, Shoichet B, Sundström M, Superti-Furga G, Taunton J, Toledo-Sherman L, Walpole C, Walters MA, Willson TM, Workman P, Young RN, Zuercher WJ.

Nat Chem Biol. 2015 Nov;11(11):887. doi: 10.1038/nchembio1115-887c. No abstract available.

PMID:
26485080
16.

The promise and peril of chemical probes.

Arrowsmith CH, Audia JE, Austin C, Baell J, Bennett J, Blagg J, Bountra C, Brennan PE, Brown PJ, Bunnage ME, Buser-Doepner C, Campbell RM, Carter AJ, Cohen P, Copeland RA, Cravatt B, Dahlin JL, Dhanak D, Edwards AM, Frederiksen M, Frye SV, Gray N, Grimshaw CE, Hepworth D, Howe T, Huber KV, Jin J, Knapp S, Kotz JD, Kruger RG, Lowe D, Mader MM, Marsden B, Mueller-Fahrnow A, Müller S, O'Hagan RC, Overington JP, Owen DR, Rosenberg SH, Roth B, Ross R, Schapira M, Schreiber SL, Shoichet B, Sundström M, Superti-Furga G, Taunton J, Toledo-Sherman L, Walpole C, Walters MA, Willson TM, Workman P, Young RN, Zuercher WJ.

Nat Chem Biol. 2015 Aug;11(8):536-41. doi: 10.1038/nchembio.1867. No abstract available. Erratum in: Nat Chem Biol. 2015 Nov;11(11):887. Nat Chem Biol. 2015 Aug;11(8):541. Roth, Brian [Corrected to Roth, Bryan] and Frederiksen, Mathias [Added].

17.

A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC.

Mohammad HP, Smitheman KN, Kamat CD, Soong D, Federowicz KE, Van Aller GS, Schneck JL, Carson JD, Liu Y, Butticello M, Bonnette WG, Gorman SA, Degenhardt Y, Bai Y, McCabe MT, Pappalardi MB, Kasparec J, Tian X, McNulty KC, Rouse M, McDevitt P, Ho T, Crouthamel M, Hart TK, Concha NO, McHugh CF, Miller WH, Dhanak D, Tummino PJ, Carpenter CL, Johnson NW, Hann CL, Kruger RG.

Cancer Cell. 2015 Jul 13;28(1):57-69. doi: 10.1016/j.ccell.2015.06.002.

18.

A687V EZH2 is a driver of histone H3 lysine 27 (H3K27) hypertrimethylation.

Ott HM, Graves AP, Pappalardi MB, Huddleston M, Halsey WS, Hughes AM, Groy A, Dul E, Jiang Y, Bai Y, Annan R, Verma SK, Knight SD, Kruger RG, Dhanak D, Schwartz B, Tummino PJ, Creasy CL, McCabe MT.

Mol Cancer Ther. 2014 Dec;13(12):3062-73. doi: 10.1158/1535-7163.MCT-13-0876. Epub 2014 Sep 24.

19.

SMYD3 links lysine methylation of MAP3K2 to Ras-driven cancer.

Mazur PK, Reynoird N, Khatri P, Jansen PW, Wilkinson AW, Liu S, Barbash O, Van Aller GS, Huddleston M, Dhanak D, Tummino PJ, Kruger RG, Garcia BA, Butte AJ, Vermeulen M, Sage J, Gozani O.

Nature. 2014 Jun 12;510(7504):283-7. doi: 10.1038/nature13320. Epub 2014 May 21.

20.

Long residence time inhibition of EZH2 in activated polycomb repressive complex 2.

Van Aller GS, Pappalardi MB, Ott HM, Diaz E, Brandt M, Schwartz BJ, Miller WH, Dhanak D, McCabe MT, Verma SK, Creasy CL, Tummino PJ, Kruger RG.

ACS Chem Biol. 2014 Mar 21;9(3):622-9. doi: 10.1021/cb4008748. Epub 2013 Dec 31.

PMID:
24304166
21.

EZH2 is required for germinal center formation and somatic EZH2 mutations promote lymphoid transformation.

Béguelin W, Popovic R, Teater M, Jiang Y, Bunting KL, Rosen M, Shen H, Yang SN, Wang L, Ezponda T, Martinez-Garcia E, Zhang H, Zheng Y, Verma SK, McCabe MT, Ott HM, Van Aller GS, Kruger RG, Liu Y, McHugh CF, Scott DW, Chung YR, Kelleher N, Shaknovich R, Creasy CL, Gascoyne RD, Wong KK, Cerchietti L, Levine RL, Abdel-Wahab O, Licht JD, Elemento O, Melnick AM.

Cancer Cell. 2013 May 13;23(5):677-92. doi: 10.1016/j.ccr.2013.04.011.

22.

Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2.

Verma SK, Tian X, LaFrance LV, Duquenne C, Suarez DP, Newlander KA, Romeril SP, Burgess JL, Grant SW, Brackley JA, Graves AP, Scherzer DA, Shu A, Thompson C, Ott HM, Aller GS, Machutta CA, Diaz E, Jiang Y, Johnson NW, Knight SD, Kruger RG, McCabe MT, Dhanak D, Tummino PJ, Creasy CL, Miller WH.

ACS Med Chem Lett. 2012 Oct 19;3(12):1091-6. doi: 10.1021/ml3003346. eCollection 2012 Dec 13.

23.

EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations.

McCabe MT, Ott HM, Ganji G, Korenchuk S, Thompson C, Van Aller GS, Liu Y, Graves AP, Della Pietra A 3rd, Diaz E, LaFrance LV, Mellinger M, Duquenne C, Tian X, Kruger RG, McHugh CF, Brandt M, Miller WH, Dhanak D, Verma SK, Tummino PJ, Creasy CL.

Nature. 2012 Dec 6;492(7427):108-12. doi: 10.1038/nature11606. Epub 2012 Oct 10.

PMID:
23051747
24.

Development and validation of reagents and assays for EZH2 peptide and nucleosome high-throughput screens.

Diaz E, Machutta CA, Chen S, Jiang Y, Nixon C, Hofmann G, Key D, Sweitzer S, Patel M, Wu Z, Creasy CL, Kruger RG, LaFrance L, Verma SK, Pappalardi MB, Le B, Van Aller GS, McCabe MT, Tummino PJ, Pope AJ, Thrall SH, Schwartz B, Brandt M.

J Biomol Screen. 2012 Dec;17(10):1279-92. doi: 10.1177/1087057112453765. Epub 2012 Aug 17.

PMID:
22904200
25.

Smyd3 regulates cancer cell phenotypes and catalyzes histone H4 lysine 5 methylation.

Van Aller GS, Reynoird N, Barbash O, Huddleston M, Liu S, Zmoos AF, McDevitt P, Sinnamon R, Le B, Mas G, Annan R, Sage J, Garcia BA, Tummino PJ, Gozani O, Kruger RG.

Epigenetics. 2012 Apr;7(4):340-3. doi: 10.4161/epi.19506. Epub 2012 Apr 1.

26.

Mutation of A677 in histone methyltransferase EZH2 in human B-cell lymphoma promotes hypertrimethylation of histone H3 on lysine 27 (H3K27).

McCabe MT, Graves AP, Ganji G, Diaz E, Halsey WS, Jiang Y, Smitheman KN, Ott HM, Pappalardi MB, Allen KE, Chen SB, Della Pietra A 3rd, Dul E, Hughes AM, Gilbert SA, Thrall SH, Tummino PJ, Kruger RG, Brandt M, Schwartz B, Creasy CL.

Proc Natl Acad Sci U S A. 2012 Feb 21;109(8):2989-94. doi: 10.1073/pnas.1116418109. Epub 2012 Feb 8.

27.

GSK1838705A inhibits the insulin-like growth factor-1 receptor and anaplastic lymphoma kinase and shows antitumor activity in experimental models of human cancers.

Sabbatini P, Korenchuk S, Rowand JL, Groy A, Liu Q, Leperi D, Atkins C, Dumble M, Yang J, Anderson K, Kruger RG, Gontarek RR, Maksimchuk KR, Suravajjala S, Lapierre RR, Shotwell JB, Wilson JW, Chamberlain SD, Rabindran SK, Kumar R.

Mol Cancer Ther. 2009 Oct;8(10):2811-20. doi: 10.1158/1535-7163.MCT-09-0423.

28.

Distinct concentration-dependent effects of the polo-like kinase 1-specific inhibitor GSK461364A, including differential effect on apoptosis.

Gilmartin AG, Bleam MR, Richter MC, Erskine SG, Kruger RG, Madden L, Hassler DF, Smith GK, Gontarek RR, Courtney MP, Sutton D, Diamond MA, Jackson JR, Laquerre SG.

Cancer Res. 2009 Sep 1;69(17):6969-77. doi: 10.1158/0008-5472.CAN-09-0945. Epub 2009 Aug 18.

29.

Kinetic analysis of teicoplanin glycosyltransferases and acyltransferase reveal ordered tailoring of aglycone scaffold to reconstitute mature teicoplanin.

Howard-Jones AR, Kruger RG, Lu W, Tao J, Leimkuhler C, Kahne D, Walsh CT.

J Am Chem Soc. 2007 Aug 22;129(33):10082-3. Epub 2007 Jul 28. No abstract available.

PMID:
17661468
30.

Staphylococcus aureus sortase transpeptidase SrtA: insight into the kinetic mechanism and evidence for a reverse protonation catalytic mechanism.

Frankel BA, Kruger RG, Robinson DE, Kelleher NL, McCafferty DG.

Biochemistry. 2005 Aug 23;44(33):11188-200.

PMID:
16101303
31.

A systematic investigation of the synthetic utility of glycopeptide glycosyltransferases.

Oberthür M, Leimkuhler C, Kruger RG, Lu W, Walsh CT, Kahne D.

J Am Chem Soc. 2005 Aug 3;127(30):10747-52.

PMID:
16045364
32.

AknT is an activating protein for the glycosyltransferase AknS in L-aminodeoxysugar transfer to the aglycone of aclacinomycin A.

Lu W, Leimkuhler C, Gatto GJ Jr, Kruger RG, Oberthür M, Kahne D, Walsh CT.

Chem Biol. 2005 May;12(5):527-34.

33.

Assembly of the SIR complex and its regulation by O-acetyl-ADP-ribose, a product of NAD-dependent histone deacetylation.

Liou GG, Tanny JC, Kruger RG, Walz T, Moazed D.

Cell. 2005 May 20;121(4):515-527. doi: 10.1016/j.cell.2005.03.035.

34.

Tailoring of glycopeptide scaffolds by the acyltransferases from the teicoplanin and A-40,926 biosynthetic operons.

Kruger RG, Lu W, Oberthür M, Tao J, Kahne D, Walsh CT.

Chem Biol. 2005 Jan;12(1):131-40.

35.

Inhibition of the Staphylococcus aureus sortase transpeptidase SrtA by phosphinic peptidomimetics.

Kruger RG, Barkallah S, Frankel BA, McCafferty DG.

Bioorg Med Chem. 2004 Jul 1;12(13):3723-9.

PMID:
15186858
36.
37.

Vinyl sulfones: inhibitors of SrtA, a transpeptidase required for cell wall protein anchoring and virulence in Staphylococcus aureus.

Frankel BA, Bentley M, Kruger RG, McCafferty DG.

J Am Chem Soc. 2004 Mar 24;126(11):3404-5.

PMID:
15025450
39.

Analysis of the substrate specificity of the Staphylococcus aureus sortase transpeptidase SrtA.

Kruger RG, Otvos B, Frankel BA, Bentley M, Dostal P, McCafferty DG.

Biochemistry. 2004 Feb 17;43(6):1541-51.

PMID:
14769030
40.
41.

Chemistry and biology of the ramoplanin family of peptide antibiotics.

McCafferty DG, Cudic P, Frankel BA, Barkallah S, Kruger RG, Li W.

Biopolymers. 2002;66(4):261-84. Review.

PMID:
12491539
43.

Functional analysis of the lipoglycodepsipeptide antibiotic ramoplanin.

Cudic P, Behenna DC, Kranz JK, Kruger RG, Wand AJ, Veklich YI, Weisel JW, McCafferty DG.

Chem Biol. 2002 Aug;9(8):897-906.

44.

Complexation of peptidoglycan intermediates by the lipoglycodepsipeptide antibiotic ramoplanin: minimal structural requirements for intermolecular complexation and fibril formation.

Cudic P, Kranz JK, Behenna DC, Kruger RG, Tadesse H, Wand AJ, Veklich YI, Weisel JW, McCafferty DG.

Proc Natl Acad Sci U S A. 2002 May 28;99(11):7384-9.

45.

Synthesis of P(1)-Citronellyl-P(2)-alpha-D-pyranosyl pyrophosphates as potential substrates for the E. coli undecaprenyl-pyrophosphoryl-N-acetylglucoseaminyl transferase MurG.

Cudic P, Behenna DC, Yu MK, Kruger RG, Szewczuk LM, McCafferty DG.

Bioorg Med Chem Lett. 2001 Dec 17;11(24):3107-10.

PMID:
11720853
46.

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